› 6zyu

X-ray diffraction
1.9Å resolution

Structure of the GluA2 ligand-binding domain (L483Y-N754S) in complex with glutamate and BPAM549

Released:
DOI: 10.2210/pdb6zyu/pdb
PDB entry 6zyu coloured by chain, front view.
PDB entry 6zyu coloured by chain, side view.
PDB entry 6zyu coloured by chain, top view.
Source organism: Rattus norvegicus
Primary publication:
Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors.
Etsè KS, Dorosz J, McLain Christensen K, Thomas JY, Botez Pop I, Goffin E, Colson T, Lestage P, Danober L, Pirotte B, Kastrup JS, Francotte P
ACS Chem Neurosci 12 2679-2692 (2021)
PMID: 34242002

Function and Biology Details

Biochemical function:
Biological process:
  • not assigned
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-148607 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Glutamate receptor 2 Chains: A, B, C
Molecule details ›
Chains: A, B, C
Length: 264 amino acids
Theoretical weight: 29.3 KDa
Source organism: Rattus norvegicus
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P19491 (Residues: 413-527, 653-797; Coverage: 30%)
Gene names: GluA2, Glur2, Gria2
Sequence domains:

Ligands and Environments

8 bound ligands:
Ligand ZN 8 x ZN
Ligand CAC 1 x CAC
Ligand ACT 5 x ACT
Ligand GLU 3 x GLU
Ligand QSZ 3 x QSZ
Ligand QSW 3 x QSW
Ligand GOL 6 x GOL
Ligand CL 5 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID29
Spacegroup: P21212
Unit cell:
a: 114.324Å b: 163.084Å c: 47.449Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.164 0.162 0.187
Expression system: Escherichia coli BL21(DE3)

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Citations

1 review citation

Diversity of AMPA Receptor Ligands: Chemotypes, Binding Modes, Mechanisms of Action, and Therapeutic Effects.
Golubeva et al. (2022)
1 other article